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目的根据银杏黄酮生物药剂学性质及其临床释药行为的特点构建银杏黄酮组分自微乳-微丸释药系统。方法根据溶解度,筛选出合适的油相、乳化剂和助乳化剂;采用水滴定法绘制伪三元相图,筛选出合适的乳化剂与助乳化剂的质量比(Km值);以粒径、Zeta电位和溶液澄明度为指标,在选定的Km值下进行混合乳化剂与油相比例的筛选;采用HPLC法测定自微乳中银杏黄酮的量;根据筛选出的制剂处方制成自微乳,再加入适当的辅料采用挤出滚圆法制成微丸;评价微丸的溶出行为。结果油相、乳化剂和助乳化剂分别为肉豆蔻酸异丙酯(IPM)、聚山梨酯-80和无水乙醇;Km值为3∶1;聚山梨酯-80和无水乙醇总质量与IPM质量比为9∶1,银杏黄酮加药量0.202 5 g,制得的自微乳粒径均小于30 nm;自微乳中银杏黄酮的量为13.32 mg/m L,以自微乳作为自黏合剂制备载药量为25%的自微乳-微丸释药系统,显著提高了银杏黄酮的溶出。结论以自微乳作为前制剂制成的微丸性质较稳定,且银杏黄酮的溶出能力得到改善。
OBJECTIVE To construct a self-microemulsion-pellet delivery system of Ginkgo flavonoids according to the characteristics of biopharmaceutics and the clinical release behavior of Ginkgetin. Methods According to the solubility, the suitable oil phase, emulsifier and co - emulsifier were screened. The pseudo - ternary phase diagram was drawn by water titration method, and the mass ratio (Km) of suitable emulsifier and co - emulsifier was screened. Zeta potential and solution clarity as an index, screening the mixture of emulsifier and oil phase under the selected Km value; determining the amount of ginkgo flavone in the self-microemulsion by HPLC method; making the self-micro Milk, and then add appropriate excipients pelletized by extrusion spheronization; evaluation pellets dissolution behavior. Results The oil phase, emulsifier and co-emulsifier were isopropyl myristate (IPM), polysorbate-80 and absolute ethanol respectively. The Km value was 3:1. The total mass of polysorbate-80 and absolute ethanol And IPM mass ratio of 9: 1, ginkgo flavone dosage of 0.202 5 g, the diameter of self-microemulsions prepared were less than 30 nm; the amount of ginkgetin from the microemulsion was 13.32 mg / m L, with self-microemulsion As a self-adhesive preparation of drug loading 25% self-microemulsion - micro-drug delivery system, significantly increased the dissolution of ginkgo flavonoids. Conclusion The pellets made with self-microemulsion as a former preparation are more stable in nature and the dissolution ability of ginkgo flavonoids is improved.